2021
DOI: 10.1016/j.chembiol.2020.10.003
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Dipyridamole Inhibits Lipogenic Gene Expression by Retaining SCAP-SREBP in the Endoplasmic Reticulum

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Cited by 21 publications
(20 citation statements)
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“…Betulin, an abundant compound in birch bark, suppresses proteolytic SREBP processing 28 . Dipyridamole, a phosphodiesterase inhibitor, blocks the ER-to-Golgi transport of the SCAP–SREBP complex independently of its phosphodiesterase inhibitor activity 29 . We have previously reported that XN, the most abundant prenylated flavonoid in hops, impairs the ER-to-Golgi translocation of the SCAP–SREBP complex by binding to Sec23/24 and blocking SCAP/SREBP incorporation into common coated protein II vesicles 18 .…”
Section: Discussionmentioning
confidence: 99%
“…Betulin, an abundant compound in birch bark, suppresses proteolytic SREBP processing 28 . Dipyridamole, a phosphodiesterase inhibitor, blocks the ER-to-Golgi transport of the SCAP–SREBP complex independently of its phosphodiesterase inhibitor activity 29 . We have previously reported that XN, the most abundant prenylated flavonoid in hops, impairs the ER-to-Golgi translocation of the SCAP–SREBP complex by binding to Sec23/24 and blocking SCAP/SREBP incorporation into common coated protein II vesicles 18 .…”
Section: Discussionmentioning
confidence: 99%
“…Moreover, immunofluorescence analysis of ERK1/2 activation confirmed that dipyridamole induced the phosphorylation of ERK1/2, which was abolished by the A 2A R antagonist SCH58261. Evidence in the literature already demonstrated that dipyridamole can exert its activity in a cAMP-independent way [ 46 ]; this interesting paper investigated the mechanism of action of dipyridamole for its known ability to inhibit lipogenic gene expression by blocking the maturation of sterol regulatory element-binding proteins (SREBPs); SREBPs are key regulators of the expression of genes coding for enzymes required for the synthesis of triglycerides and cholesterol. In their paper, the authors concluded that the above-mentioned effect was not depending on cAMP, but they did not investigate other cellular signaling (e.g., that elicited by A 2A R).…”
Section: Discussionmentioning
confidence: 99%
“…More recent discoveries uncovered the heterogeneity of metabolic reprogramming in cancer cells to also include increases in oxidative phosphorylation and the use of alternative carbon sources (i.e., glutamine, fatty acids, and serine). Various studies have revealed a metabolic regulation system between cancer cells, immune cells, and stroma and have demonstrated the targetability of these metabolic shifts in preventing disease progression (151)(152)(153)(154)(155)(156)(157)(158). Surprisingly, studies have also revealed regulation and correlation between metabolic shifts and cytoskeletal proteins in cancer.…”
Section: Targeting Cytoskeletal and Metabolic Connectionsmentioning
confidence: 99%